GW-501519: GW501516 is a selective agonist (activator) of the PPARo receptor. (Peroxisome proliferator-activated receptor delta.) It display high affinity (k =1nM) and potency (EC50 = 1 nM) for PPARo with > 1000 fold selectivity over PPARo and PPARy. In rats, binding of GW501516 to PPARδ recruits th coactivator PGC-1a. The PPARδ/coactivator complex in turn upregulates the expression of proteins involved in energy expenditure.[34] Furthermore, in rats treated with GW501516, increased fatty acid metabolism in skeletal muscle and protection against diet-induced obesity and type II diabetes was observed. In obese rhesus monkeys, GW501516 increased high density lipoprotein (HDL) and lowered very low density lipoprotein (VLDL)
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